Industry News

27 November 2023

DEL for Covalent Ligand Discovery

Although many covalent drugs were serendipitously discovered historically, covalent inhibitors were in general discouraged due to the concerns over their interference with biological assays and potential lack of selectivity. Over the past decades, rational design of covalent inhibitors has gained traction and garnered increased interest, particularly due to their stronger potency, prolonged target engagement, increased selectivity, and effectiveness to some drug-resistance mutants to reversible inhibitors.
14 November 2023

DNA-Encoded Library (DEL) for Compound Optimization & Expansion

DNA-encoded library (DEL) technology represents a revolutionary method in drug discovery. Unlike conventional approaches, DEL enables unparalleled exploration of chemical space, leading to the rapid identification of novel potent compounds.
03 November 2023

Extended Nucleic Acid (exNA): A Novel, Biologically Compatible Backbone that Significantly Enhances Oligonucleotide Efficacy in vivo.
13 September 2023

DEL for Enzymes with Specific Mode of Action (MoA)

Enzymes are arguably the most ideal targets for small molecule drugs, owing to their involvement in chemical reaction catalysis and the better ligandability of the binding pockets.
25 August 2023

DEL for Protein-Protein Interaction

Protein-protein interactions (PPI) are physical and chemical contacts between two or more protein molecules. As a fundamental aspect of almost all biological processes, any interference of the sophisticated PPI network could result in potential physiological disorder or disease.
15 August 2023

DEL for RNA

While proteins have traditionally been the primary target class for drug discovery, the landscape is rapidly evolving.
07 August 2023

DEL for DNA- and RNA-Binding Proteins

While DNA-encoded library (DEL) selection has been applied to a variety of targets with multiple candidates progressed into different stages of drug development, the utilization of DEL in DNA- and RNA-binding proteins remains questionable. This is largely due to the fact that each DEL compound contains a long stretch of DNA barcode, which when used to screen against DNA- or RNA- binding proteins (transcription factors, DNA polymerases, helicases, DNases, RNases, chromatin modifying complexes, etc.) , would lead to significant false positives.
04 August 2023

DEL for GPCRs

G protein coupled receptors (GPCRs) are a family of multi-transmembrane proteins with typical 7 transmembrane regions. Many marketed drugs are known to target GPCRs.
31 July 2023

DEL for Protein Degradation

Protein degraders (most popularly known as PROTAC or Molecular Glue) utilize an event-driven process, recruit protein of interest (POI, or targeted protein) and E3 ligase directly or indirectly, induce poly-ubiquitination of POI and subsequent proteasome-mediated degradation. Unlike protein inhibitors, protein degraders do not require inhibitory activity to the protein, therefore, this modality of therapeutics applies to broader target classes including undruggable proteins, scaffold proteins, mutant proteins and etc.
04 December 2021

Richard Lerner Remembrance

It is with great sadness that we hear of the passing of Professor Richard A Lerner. Richard served as the director of the Scripps Research Institute from 1991 until 2012, and in 1992 published the seminal paper in PNAS describing the concept of recording a series of chemical transformations by a DNA “code” with his Scripps colleague and Nobel laureate Dr. Sidney Brenner (1927-2019).

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